Medicinal inorganic chemistry – challenges, opportunities and guidelines to develop the next generation of radioactive, photoactivated and active site inhibiting metal-based medicines

Abstract

Medicinal inorganic chemistry is a burgeoning subfield of medicinal chemistry that focuses on the development of metal-based diagnostic and therapeutic agents.

Impact of the zinc complexation of polytopic polyaza ligands on the interaction with double and single stranded DNA/RNA and antimicrobial activity

“…13 Moreover, polynuclear complexes can show a synergetic and/or complementary effect between the metals when binding to biomolecules such as DNA, RNA, lipids or proteins as well as present additional functionalities such as imaging. 14 Our team and other groups have extensively investigated polynuclear complexes, with particular attention to first-row metals such as zinc, copper and manganese. [15][16][17][18][19][20][21] Recently, we described how the formation of binuclear complexes modulated the interaction of several ligands with DNA/RNA.…”

“…13 Moreover, polynuclear complexes can show a synergetic and/or complementary effect between the metals when binding to biomolecules such as DNA, RNA, lipids or proteins as well as present additional functionalities such as imaging. 14…”

Interaction of Radiopharmaceuticals with Somatostatin Receptor 2 Revealed by Molecular Dynamics Simulations

“…Most efforts of modern medicine are addressed toward personalized medicine, in which each patient is treated according to the molecular features of the disease of interest. , In this contest, radiopharmaceuticals have been extensively used to specifically target unhealthy tissues. , According to the decay properties of the radionuclide, compounds can be employed for diagnostic or therapeutic purposes, or both (theranostics) . Radionuclides emitting γ or β+ ( e.g.…”

“…7 In some cases, the radionuclide emits both β+ and β-( 64 Cu), or γ and β-( 177 Lu), making their use suitable for theranostics. 4,8 However, the inability to precisely quantify the radiation doses supplied to tumors and normal tissues has been one of the main drawbacks of radionuclide-based treatments. For example, 111 In decays by electron capture emitting relatively high-energy γ photons with a half-life (t 1/2 ) of 67.2 h, resulting in suboptimal imaging resolution and high radiation exposure in patients, which is even more pronounced when using shortlived isotopes, such as 68 Ga (t 1/2 = 1.13 h).…”

“…1,2 In this contest, radiopharmaceuticals have been extensively used to specifically target unhealthy tissues. 3,4 According to the decay properties of the radionuclide, compounds can be employed for diagnostic or therapeutic purposes, or both (theranostics). 5 Radionuclides emitting γ or β+ (e.g., 111 In and 68 Ga) are exploited for imaging with single-photon emission computed tomography (SPECT) and positron emission tomography (PET), respectively, while those emitting βor α (e.g., 177 Lu and 211 At) are used for therapeutic treatments.…”